> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/defactinib-93d3f8e7-960f-4e54-9e6e-fd0a1504d053
> Record changed: 2026-11-04

# Defactinib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3137331)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3137331)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3137331)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3137331)

**Drug name**

Defactinib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3137331)

**Molecular weight**

510.5

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3137331)

**Structure (SMILES)**

CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3nccnc3N(C)S(C)(=O)=O)n2)cc1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3137331)

### Other names (20)

- defacitinib
- DEFACITINIB
- defactinib
- Defactinib
- DEFACTINIB
- DEFACTINIB (VS-6063)
- defactinib \[INN\]
- DEFACTINIB \[USAN\]
- Defactinib \[WHO-DD\]
- defactinib hydrochloride
- DEFACTINIB HYDROCHLORIDE
- defactinib inn
- defactinib usan
- defactinib vs 6063
- defactinib who dd
- pf 04554878
- PF-04554878
- vs 6063
- Vs-6063
- VS-6063

## Identifiers

**CAS registry numbers**

- 1073154-85-4

**ChEMBL ID**

CHEMBL3137331

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3137331)

**InChIKey**

FWLMVFUGMHIOAA-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3137331)

**PubChem compound IDs**

- 25117126

**FDA ingredient codes (UNII)**

- 53O87HA2QU

### RxNorm IDs (RxCUI) (2)

- 2714501
- 2714502

## Regulatory information

### Other regulatory facts

**Patents**

0

**Designations**

1

**First in class**

No

**Fast track**

No

**Breakthrough designation**

No

**Orphan designation**

No

**Priority review**

No

**Orphan exclusivity**

No

**Accelerated approval**

No

## Pharmacology

### Drug classification

**Pharmacology name**

defactinib

**Type**

Synthetic organic

**Drug name stem**

\-tinib

**Approval recorded by Guide to Pharmacology**

Yes

### Mechanisms of action (3)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
large tumor suppressor kinase 1

**Gene symbol**  
LATS1

**Protein identifier**  
O95835

**Median affinity**

5.04

**Affinity units**  
pKd
- **Mechanism**  
Focal adhesion kinase 1 inhibitor

**Action type**  
Inhibitor

**Target**  
Focal adhesion kinase 1

**Protein identifier**  
Q05397
- **Mechanism**  
Protein tyrosine kinase 2 beta inhibitor

**Action type**  
Inhibitor

**Target**  
Protein-tyrosine kinase 2-beta

**Protein identifier**  
Q14289

### Open Targets mechanisms (2)

- **Mechanism**  
Focal adhesion kinase 1 inhibitor

**Action type**  
Inhibitor

**Target**  
Focal adhesion kinase 1
- **Mechanism**  
Protein tyrosine kinase 2 beta inhibitor

**Action type**  
Inhibitor

**Target**  
Protein-tyrosine kinase 2-beta

### Investigated indications (13)

- **Condition**  
Carcinoma, Endometrioid

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000466

**Subject identifier**  
D018269
- **Condition**  
Glioblastoma

**Highest recorded phase**

0.5

**Condition identifier**  
EFO:0000519

**Subject identifier**  
D005909
- **Condition**  
Melanoma

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000756

**Subject identifier**  
D008545
- **Condition**  
Mesothelioma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000770

**Subject identifier**  
D008654
- **Condition**  
Pancreatic Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0002618

**Subject identifier**  
D010190
- **Condition**  
Thyroid Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0002892

**Subject identifier**  
D013964
- **Condition**  
Carcinoma, Non-Small-Cell Lung

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003060

**Subject identifier**  
D002289
- **Condition**  
Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
MONDO:0004992

**Subject identifier**  
D009369
- **Condition**  
Carcinoma, Pancreatic Ductal

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0005184

**Subject identifier**  
D021441
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0005575

**Subject identifier**  
D015179
- **Condition**  
Ovarian Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0008170

**Subject identifier**  
D010051
- **Condition**  
Lung Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0008903

**Subject identifier**  
D008175
- **Condition**  
Genital Neoplasms, Female

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0021148

**Subject identifier**  
D005833

### Open Targets indications (36)

- **Condition identifier**  
EFO\_0000519
- **Condition identifier**  
EFO\_0000588

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000770

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003060
- **Condition identifier**  
EFO\_0003860
- **Condition identifier**  
EFO\_1000359

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0001056

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0001657

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0004992

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005061

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005062

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005065

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005105

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005112

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005184

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005192

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005211

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005575

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0006047

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0006292

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0006468

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008170

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008170

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0009693

**Highest recorded phase**  
2

And 11 more, listed on the interactive page.

### Trial references (20)

- NCT00787033  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00787033)
- NCT01943292  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01943292)
- NCT01778803  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01778803)
- NCT02943317  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02943317)
- NCT03875820  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03875820)
- NCT04625270  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04625270)
- NCT06072781  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06072781)
- NCT06394804  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06394804)
- NCT01870609  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01870609)
- NCT04201145  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04201145)
- NCT01951690  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01951690)
- NCT04620330  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04620330)
- NCT02546531  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02546531)
- NCT04331041  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04331041)
- NCT03727880  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03727880)
- NCT05787561  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05787561)
- NCT05798507  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05798507)
- NCT06007924  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06007924)
- NCT06194929  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06194929)
- NCT06369259  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06369259)

## Chemical properties

**Hydrogen bond acceptors**

9

**Hydrogen bond donors**

3

**Polar surface area**

142.1

**Calculated partition coefficient (ALogP)**

2.4

**Calculated partition coefficient (XLogP)**

1.4

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

1

**Rotatable bonds**

8

**Heavy atoms**

35

**Molecular formula**

C20H21F3N8O3S

**Monoisotopic mass**

510.14094222

**Natural product**

No

## Evidence counts

**Recorded assays**

3,238

**Active assays**

270

### Active assay types (2)

- Confirmatory
- Screening

## Related records

### Trials (39)

- 5G-RUBY: Avutometinib and Defactinib in Malignant Brain Tumours
- [A Phase 1/2 Study of VS-7375 in Patients With KRAS G12D-Mutated Solid Tumors](https://trialight.com/data/trial/a-phase-1-2-study-of-vs-7375-in-patients-with-kras-g12d-2a83cb8c-fe8d-4b5c-88de-0eebb2025cdc.md)
- A Phase 2 Study of Avutometinib (VS-6766) Plus Defactinib
- A Phase I, Open-label Study of Absorption, Metabolism, and Excretion of Defactinib (VS-6063) in Healthy Male Subjects
- A Study of Avutometinib (VS-6766) + Defactinib (VS-6063) in Recurrent Low-Grade Serous Ovarian Cancer
- A Study of Avutometinib (VS-6766) + Defactinib in Recurrent KRAS G12V, Other KRAS and BRAF Non-Small Cell Lung Cancer
- A Study of Avutometinib (VS-6766) and Defactinib in People With Mesonephric Gynecologic Cancer
- A Study of Avutometinib (VS-6766) v. Avutometinib (VS-6766) + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer With and Without a KRAS Mutation
- A Study of Avutometinib + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer in Japanese Patients
- A Study of Avutometinib and Defactinib in People With Thyroid Cancer
- A Study of Avutometinib, Defactinib, and Letrozole in People With Low-Grade Serous Ovarian Cancer
- A Study Of PF-04554878 In Patients With Advanced Non-Hematologic Malignancies
- Avutometinib and Defactinib in Diffuse Gastric Cancer
- Combination of Avutometinib and Defactinib for Treatment of Relapsed, Refractory, Metastatic, or Unresectable Malignant Peripheral Nerve Sheath Tumor
- Combined Evaluation of Epigenetic and Sensitising Therapy in AML and MDS
- Continued Access to Avutometinib in Combination With Defactinib in Patients With Recurrent Low-Grade Serous Ovarian Cancer (LGSOC)
- Defactinib and Avutometinib, With or Without Encorafenib, for the Treatment of Patients With Brain Metastases From Cutaneous Melanoma
- Defactinib Combined With Pembrolizumab and Gemcitabine in Patients With Advanced Cancer
- Defactinib, Avutometinib and Nivolumab for the Treatment of Anti-PD1 Refractory LKB1-Mutant Advanced Non-Small Cell Lung Cancer
- Identification of Treatment Concentrations of Defactinib or VS-6766 for the Treatment of Patients With Glioblastoma

### In development for (32)

- [Acute myeloid leukemia](https://trialight.com/data/condition/acute-myeloid-leukemia-b0971a7a-c18d-544e-bd7f-b1a13b9caa30.md) Phase 1
- [Brain cancer](https://trialight.com/data/condition/brain-cancer-f8f25210-90da-5298-8c6b-4f230fcb45cd.md) Phase 1
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 1
- [Chronic myelomonocytic leukemia](https://trialight.com/data/condition/chronic-myelomonocytic-leukemia-202fe88e-7b5d-5022-b6d2-095cac037e8e.md) Phase 1
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 2
- [Differentiated thyroid carcinoma](https://trialight.com/data/condition/differentiated-thyroid-carcinoma-d7c5bae1-a4cb-5587-998c-99d7ccc3ba9a.md) Phase 2
- [Endometrial cancer](https://trialight.com/data/condition/endometrial-cancer-4da2a0bc-7943-502b-a698-cc2beccbed8c.md) Phase 1
- Endometrioid adenocarcinoma Phase 1
- Exocrine pancreatic carcinoma Phase 2
- [Female reproductive system neoplasm](https://trialight.com/data/condition/female-reproductive-system-neoplasm-a546c16a-5a0e-51fa-bf62-79ed8ecf0059.md) Phase 2
- [Gastric cancer](https://trialight.com/data/condition/gastric-cancer-3c1e2785-2672-5b3e-afce-9335f684c159.md) Phase 2
- [Gastric neoplasm](https://trialight.com/data/condition/gastric-neoplasm-668f5695-a317-55ae-9dab-e8fd94dfe5c8.md) Phase 2
- Glioblastoma Early phase 1
- [Lung adenocarcinoma](https://trialight.com/data/condition/lung-adenocarcinoma-1cff3624-1dd5-5076-89a7-1f8a28c087a6.md) Phase 2
- [Lung cancer](https://trialight.com/data/condition/lung-cancer-c4ca1fe0-9b3d-5957-a668-2d6cf26bd16a.md) Phase 2
- [Lymphoma](https://trialight.com/data/condition/lymphoma-de4db685-7419-5e0e-b958-4591ffd69d43.md) Phase 2
- Malignant mesothelioma Phase 1
- [Malignant pancreatic neoplasm](https://trialight.com/data/condition/malignant-pancreatic-neoplasm-5dd0b53e-5962-50ea-a2e5-cf2444bd0485.md) Phase 2
- Malignant pleural mesothelioma Phase 2
- [Melanoma](https://trialight.com/data/condition/melanoma-457e9de6-dcd9-56fb-be48-0290fb4386ef.md) Phase 1

### Targets (3)

- [LATS1](https://trialight.com/data/target/lats1-23798e46-1bc7-5a8c-9e1d-e5441c833025.md)
- [PTK2](https://trialight.com/data/target/ptk2-b2d6adf1-0ce8-54d4-b3f7-44b2db6f9811.md) Focal adhesion kinase 1 inhibitor
- [PTK2B](https://trialight.com/data/target/ptk2b-f32e1aa9-5335-57b8-9c94-c2e17dec2c61.md) Protein tyrosine kinase 2 beta inhibitor

---

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